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Assay Detail

CHEMBL3611488

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PI3Kgamma (unknown origin)
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Fairhurst RA, Imbach-Weese P, Gerspacher M, Caravatti G, Furet P, Zoller T, Fritsch C, Haasen D, Trappe J, Guthy DA, Arz D, Wirth J.
Bioorg Med Chem Lett (2015) 25 : 3569 -3574
PubMed 26206504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.61 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2397186 1 6.64
CHEMBL2396661 ALPELISIB 4.0 1 6.60
CHEMBL2071330 1 6.06
CHEMBL3608321 1 5.92
CHEMBL3608927 1 5.60
CHEMBL3609545 1 5.54
CHEMBL3609542 1 5.52
CHEMBL3608929 1 5.30
CHEMBL3609538 1 5.21
CHEMBL3609537 1 5.20
CHEMBL3218581 1 5.10
CHEMBL3608931 1 5.10
CHEMBL3608930 1 5.08
CHEMBL3609539 1 -
CHEMBL3609536 1 -
CHEMBL2071336 1 -
CHEMBL3609541 1 -
CHEMBL3609543 1 -
CHEMBL3609544 1 -
CHEMBL3608924 1 -
CHEMBL3608925 1 -
CHEMBL3608926 1 -
CHEMBL3608936 1 -
CHEMBL3608928 1 -
CHEMBL3608932 1 -
CHEMBL3608933 1 -
CHEMBL3608934 1 -
CHEMBL3609540 1 -
CHEMBL3608935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2397186 IC50 = 230.0 nM 6.64
CHEMBL2396661 ALPELISIB IC50 = 250.0 nM 6.60
CHEMBL2071330 IC50 = 870.0 nM 6.06
CHEMBL3608321 IC50 = 1200.0 nM 5.92
CHEMBL3608927 IC50 = 2500.0 nM 5.60
CHEMBL3609545 IC50 = 2900.0 nM 5.54
CHEMBL3609542 IC50 = 3000.0 nM 5.52
CHEMBL3608929 IC50 = 5000.0 nM 5.30
CHEMBL3609538 IC50 = 6100.0 nM 5.21
CHEMBL3609537 IC50 = 6300.0 nM 5.20
CHEMBL3218581 IC50 = 8000.0 nM 5.10
CHEMBL3608931 IC50 = 7900.0 nM 5.10
CHEMBL3608930 IC50 = 8300.0 nM 5.08
CHEMBL3609539 IC50 > 10000.0 nM -
CHEMBL3609536 IC50 - -
CHEMBL2071336 IC50 > 10000.0 nM -
CHEMBL3609541 IC50 > 10000.0 nM -
CHEMBL3609543 IC50 > 10000.0 nM -
CHEMBL3609544 IC50 - -
CHEMBL3608924 IC50 - -
CHEMBL3608925 IC50 - -
CHEMBL3608926 IC50 - -
CHEMBL3608936 IC50 > 10000.0 nM -
CHEMBL3608928 IC50 > 10000.0 nM -
CHEMBL3608932 IC50 > 10000.0 nM -
CHEMBL3608933 IC50 > 10000.0 nM -
CHEMBL3608934 IC50 > 10000.0 nM -
CHEMBL3609540 IC50 - -
CHEMBL3608935 IC50 - -